Lonidamine is an orally-available, indazole-based inhibitor of glycolysis by the inactivation of hexokinase. Lonidamine is believed to increase apoptosis and in in vitro models has displayed markers of mitochondrial membrane depolarization, cytochrome C release, phosphatidylserine externalization, and DNA fragmentation. In support of apotosis induction, caspase activity was found to be enhanced by Lonidamine in LNCaP cells. (1)

In separate studies, lonidamine was found to act of mitochondra to induce apoptosis by dissipating the inner transmembrane potential and the release of key apoptotic factors. (2)